发明公开
- 专利标题: ANTITUMOR WIRKSAME 2-ALKOXYESTRADIOLSULFAMATE
- 专利标题(英): Anti-tumour 2-alkoxyestradiol sulfamates
- 专利标题(中): 抗氧剂WIRKSAME 2-ALKOXYESTRADIOLSULFAMATE
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申请号: EP02762422.0申请日: 2002-08-01
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公开(公告)号: EP1418921A1公开(公告)日: 2004-05-19
- 发明人: SCHERLITZ-HOFMANN, Ina , HOFFMANN, Jens , HILLISCH, Alexander , UNGER, Eberhard , NEUMANN, Tobias , SCHWARZ, Sigfrid , PETERS, Olaf , MICHEL, Thomas
- 申请人: Schering AG
- 申请人地址: Müllerstrasse 178 13353 Berlin-Wedding DE
- 专利权人: Schering AG
- 当前专利权人: Schering AG
- 当前专利权人地址: Müllerstrasse 178 13353 Berlin-Wedding DE
- 代理机构: Ziebig, Marlene, Dr. Dipl.-Chem.
- 优先权: DE10139494 20010813
- 国际公布: WO2003015792 20030227
- 主分类号: A61K31/565
- IPC分类号: A61K31/565 ; C07J31/00 ; A61P35/00
摘要:
The invention relates to the use of 2-alkoxyestrogen sulfamates of general formula (I) for producing a medicament for the treatment of tumorous diseases, which are positively influenced by the inhibition of tubulin polymerisation. In said formula, R?1 and R2¿ independently of one another represent H, methyl, C¿1?-C4 acyl or benzyl, R?3¿ represents C¿1?-C4 alkyl, or a group of formula CnFmHo, where n = 1, 2, 3, 4, 5 or 6, m > 1 and m + o = 2n + 1, R?4 and R5¿ independently represent H, or together represent a methylene group or an additional bond, R6 represents H and R7 represents OH, OC¿1?-C4 alkyl, OC1-C11 acyl or OSO2NR?1R2¿, whereby in the B and C ring of the steroid skeleton the broken lines can additionally represent up to two double bonds. The inventive compounds are characterised by a 2-alkoxy substitution in conjunction with a 17-hydroxy substitution. They exhibit the specific activity of inhibiting tubulin polymerisation and can be used, for example, for treating prostatic carcinoma.
公开/授权文献
- EP1418921B1 ANTITUMOR WIRKSAME 2-ALKOXYESTRADIOLSULFAMATE 公开/授权日:2007-10-03
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